Owing to the outbreak of fatal diseases that require searching for new compounds with high activity and/or novel action mechanisms, screening for promising sources of biologically active compounds that fulfill the current needs of humanity is a matter of life and death. Fungi generally and endophytic ones specifically represent future factories and potent biotechnological tools for production of bioactive natural substances, which could extend healthy life span of humanity (as done by penicillin from centuries), and are considered promising alternatives for some high costly produced chemicals and drugs. The present review highlights some bioactive secondary metabolites, produced by fungal endophytes, involved in medical, pharmaceutical, agricultural, and industrial applications.

Epilepsy remains one of the most challenging diseases worldwide. According to the WHO, ∼50 million people around the world experience epilepsy with all its implications on the patient’s overall quality of life and social life as well as social stigma. The causes of epilepsy are mostly unknown. Epilepsy treatment is considered as a huge economic burden on the patient and health care systems. This review aimed to shed light on the different types of epilepsy, the different mechanisms of action of the most novel antiepileptic drugs in the market, as well as the current antiepileptic drugs under investigation and undergoing clinical trials.

Changes in lifestyle have led to increased prevalence of many central nervous system diseases and disorders. The delivery of drug to the brain as well as to bone marrow has been a major challenge owing to the selectivity of physiological barriers. Several efforts have been made with different techniques to overcome such barriers for effective delivery of drugs to these two targets. These include chemical modification of the drug, receptor-mediated entry, nanotechnology-based drug transport, osmotic disruption, etc. The commonly used approaches, for delivery of drugs to the bone, are drug depots and targeted systemically delivered carriers. However, delivery of drugs to the brain and bone is highly challenging. Although there are various techniques for the delivery of drugs to the brain and the bone, the success rate of such techniques need crucial monitoring. Moreover, the techniques should be assessed for their safety, risks, and benefits to the patients and associated consequences. It is of utmost important that any delivery systems should have no significant effect on the normal healthy functions of the brain and the bone. Depending on the physico-chemical characteristics of a drug, the best method of drug delivery should be selected. Such techniques are discussed in this article.

Background and objectives In the Egyptian flora, the genus Asphodelus was formally placed in Liliaceae family and recently is ranked as a separate family; Asphodelaceae. Asphodelus aestivus Brot. is the one of the five Asphodelus spp. distributed wild in Egypt; it grows on rocky or sandy ground and in dry grasslands. Therefore, this study aims to investigate the chemical constituents of A. aestivus compared with those reported in the species of families Liliaceae s.l. and Asphodelaceae to evaluate their chemosystematic relationship.
Materials and methods The chemical components of the defatted hydroalcoholic extract of A. aestivus were analyzed using different chromatographic and spectral techniques.
Results and conclusion A total of 13 flavonoid compounds were isolated from A. aestivus. They are identified as kaempferol (1), kaempferol 7-O-β-glucopyranoside (2), kaempferol 3-O-(6′-α-rhamnopyranosyl)-β-glucopyranoside-7-O-α-rhamnopyranoside (3), apigenin (4), apigenin 7-O-β-glucopyranoside (5), luteolin (6), luteolin 7-O-β-glucopyranoside (7), vitexin (8), isovitexin (9), apigenin 6, 8 di-C-β-glucopyranoside (10), saponarin (11), orientin (12), and isoorientin (13). Except for compounds 9 and 13, all compounds were isolated for the first time from A. aestivus. A. aestivus is characterized by flavones, flavonols, and flavone C-glycosides. It is thus different from other species of Liliaceae s.l. which are characterized by either flavones and flavone C-glycosides or flavonols and flavone C-glycosides, supporting the placement of the genus Asphodelus in a distinct family (Asphodelaceae).

Background and objective Turmeric is a widely known spice that comes from the roots of the plant.
Materials and methods Phenylpyridazine derivatives based on curcumin (Turmeric, Curcuma longa) were synthesized via diazotization of curcumin with appropriate aryl amine derivatives such as p-nitro aniline, p-amino benzoic acid and m-amino benzoic acid. The used fabrics were bleached poplin cotton fabric, mill scoured natural silk fabric and mill scoured pure wool fabric. Effects of mordant and fastness properties for treated fabric were evaluated.
Results and conclusion The structure of the obtained diazonyl derivatives has been confirmed from their spectroscopic data (ultraviolet, IR and 1H-NMR). Comparable novel curcumin derivatives with curcumin have been investigated with and/or without simultaneous mordanting for natural fibres (cotton, silk and wool). A variety of colours have been obtained by using different mordants. The fastness properties of the dyed fabrics to washing and light fastness were improved.

Background and objectives Although there are several toxicological studies on aspartame (ASP), its histopathological effects on the liver have received little attention. Natural marjoram [Origanum majorana (OM)] is extensively studied for its ability to protect cells from damages. The present study was to evaluate the chronic effects of ASP, and marjoram as well as the protective effect of aqueous extract of marjoram leaves (OM) against ASP-induced liver toxicity.
Materials and methods Seventy-two female albino rats (180±20 g) were divided into nine groups: G1 as a control, G2 and G3 received ASP, G4 and G5 were administrated water extract OM, and G6, G7, G8, and G9 were treated with ASP+OM. Serum glutamate oxaloacetate transaminase, glutamate pyruvate transaminase, vascular endothelial growth factor levels, and histological examination of the liver tissues were detected for all groups.
Results and conclusion ASP caused a significant increase in glutamate oxaloacetate transaminase, glutamate pyruvate transaminase, and vascular endothelial growth factor levels. A combination of OM (100 or 300 mg/rat) with ASP (50 or 100 mg/rat) improved most of the previous parameters. Histological examination of the liver showed some abnormality, but no significant morphological changes in G6, G7, G8, and G9. The treated rats (G2 and G3) showed hepatic fibrosis, nuclear changes, hepatocyte degeneration disruption hepatic cords, and cytoplasmic vacillations. ASP groups treated with OM showed improvement of many hepatic changes. Thus, OM may have a protective effect on ASP hepatotoxicity.

Background Type 2 diabetes (T2D) is hallmarked by insulin resistance and pancreatic gradual islet β-cell dysfunction and hyperglycemia. Consumption of large quantities of high-fat diet (HFD) activates the caspase-pathway. This leads to apoptotic degradation of pancreatic β-cell and eventually progression to T2D or worsening of diabetes.
Aims We aimed to assess the antidiabetic effects of aspirin when administered at low doses on insulin sensitivity and glucose uptake.
Materials and methods A rat model fed HFD has been reported as an approved model of T2D. A total of 40 animals were assigned into four groups: controlled diet, HFD, controlled diet with aspirin, and HFD with aspirin. Hyperglycemia was confirmed by estimating the blood glucose levels. The diabetic rats were orally treated with low dose of aspirin 20 mg/kg body weight, for 70 days. At the end of the experiment, some biochemical parameters, the oxidative stress, and gene expression levels were quantified.
Results Current data indicated that aspirin improved different physiological and immunological parameters. These include reduction of low-density lipoprotein and total cholesterol and improved glucose uptake via up-regulation of GLUT4 expression. Moreover, aspirin reduced fat peroxidation and obliterated hemeoxygenase-1-dependent fat down-regulation and reestablished the expression of LUT4 and hemeoxygenase-1 to the basal level.
Conclusions In conclusion, this study confirmed the anti-inflammatory effect of aspirin and suggested that low-dose aspirin enhanced the metabolism of glucose and increased insulin sensitivity by suppression of inflammation and oxidative stress.

Background and objectives Fused triazine derivatives are known to be a very important class of compounds that have significant biological activities. Also, they showed a broad spectrum against leukemic cell lines and cancer cells. Our objective after such a study is, on one hand, to shed some light on the synthesis of triazolotriazine and hydrazone derivatives from the thiothymine compound and, on the other hand, to explore the biological activity of the isolated products from such reactions.
Materials and methods Reaction of thiothymine 3 and hydrazonoyl chloride 1 in refluxing chloroform in the presence of triethylamine yielded triazolotriazine derivatives 11. The hydrazino derivative 14 underwent condensation reactions with aldehydes, pyruvic acid, ethyl pyruvate, and ketones to give the corresponding hydrazone derivatives 15 and 16, respectively. Antimicrobial activities of some newly synthesized compounds were studied using the diffusion plate method.
Results and conclusion Both antibacterial and antifungal activities of the new synthesized compounds 14, 15h, and 16a–d were studied. Also, the minimum inhibitory concentration values for the highly efficient antibacterial compounds using the most sensitive microorganisms were determined.

Studies on the microbial decontamination of Egyptian bee pollen by γ radiation

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AS Hosny, FM Sabbah, ZE EL-BazzaDOI:10.4103/epj.epj_19_18

Objective Bee pollen are used as health food ingredients, but may be subjected to microbial contamination; γ radiation technology can offer the process of microbial decontamination as a means of achieving microbiological safety limits.
Materials and methods Thirty bee pollen samples were collected from Egyptian markets. Detection of contamination and the microbial counts were carried out on nutrient and Sabouraud’s agar media for bacteria and fungi, respectively, using the aerobic plate technique. Identification of bacteria was carried out by biochemical methods and analytical profile index. Moreover, identification of fungi was carried out morphologically and microscopically.
Results and conclusion The order of bacterial contamination was Gram-positive rods>Gram-negative rods>Gram-positive cocci. The order of fungal contamination is Penicillium spp.>Aspergillusflavus>Aspergillus niger>Aspergillus ochracueus. Only three strains of A. flavus could produce aflatoxin B1. The microbial counts of bee pollen samples decreased with increasing γ radiation doses. The most radio-resistant bacteria that were isolated at 5.0 kGy were identified as Bacillusmegaterium, Bacillus pumilis and Bacillus subtilis. The most radio-resistant fungi were identified as Penicillium chrysogenum, Penicillium expansum and Penicillium corylophilum. Using of γ radiation can decrease the bioburden in bee pollen, and eliminate pathogenic microorganisms including fungi, which can produce carcinogenic aflatoxins.

Background and objectives Naproxen (S)-6-methoxy-α-methyl-2-naphthaleneacetic acid (or sodium salt) belongs to a group of pharmaceuticals known as NSAIDs. The aim of this study is to describe the construction and performance characteristics of naproxen (NAP) screen-printed sensors.
Materials and methods Various sensor fabrication protocols have been applied including bulk modification with NAP-surfactants ion pairs (IPs), in-situ modification with ion pairing agents and soaking the plain electrode in IP suspension solutions. Qualitative and quantitative matrix composition optimization was done referring to the effect of modifier and plasticizer. Conductometric measurements were performed for the determination of the solubility products of NAP-surfactants ion associates.
Results and conclusion The fabricated sensors showed Nernstian compliance in the concentration range from 10−7 to 10−2 mol/l (detection limit 8.0×10−8 mol/l) with fast response time (4 s) and long operational lifetime (3 months). The developed electrodes have been successfully applied for the potentiometric determination of NAP in pure and dosage forms under standard addition and potentiometric titration conditions with average recoveries agreeable with the reported official methods. The solubility products of various NAP-IPs were determined conductometrically.

Background The antioxidant activity of some benzofuran and 2H-pyran-2-one derivatives of naturally occurring khellin and visnagin was theoretically investigated using a quantum chemical method, density functional theory. These molecules possess a variety of biological and pharmacological activities including antioxidant activity.
Materials and methods The calculations were carried out using Gaussian 03 computational package in gas phase with the purpose of obtaining the intrinsic properties of the molecules studied, free of any interaction. The geometries of neutral species and their respective radicals and radical cations were optimized using PM3 and density functional theory/B3LYP calculations with cc-pVDZ basis set.
Results As they possess O-H, N-H, or both O-H and N-H bonds, we chose to investigate theoretically their antioxidant activity via H-atom transfer or single electron transfer pathway. In the gas phase, the ionization potential, the highest occupied molecular orbital (HOMO), bond dissociation energies of hydroxyl group O-H and N-H [bond-dissociation enthalpy (BDE)O-H–BDEN-H], and spin density distribution are carried out. Molecule 14 showed potential antioxidant activity as BDE for the N-H bond was found to be 84.71 and for the O-H bond was 85.32, whereas the ionization potential was 6.26 and the EHOMO was 5.39.
Conclusion Based on the antioxidant activities of 15 derivatives of naturally occurring khellin and visnagin, they were found to be potent antioxidant compounds comparable to quercetin or vitamin C.

Background and objective The discovery of novel naturally occurring antimicrobial agents is one of the most promising approaches for overcoming the growing threat of antibiotic-resistant pathogens. Venomous animals from different ecological niches and taxonomic groups have recently gained attention in the search for new antimicrobials to treat infectious diseases. Therefore, the main aim of the present study was to investigate the antimicrobial activity of Orient hornet venom.
Materials and methods Different concentrations of wasp venom were tested for their antimicrobial effect against two gram-negative bacteria (Salmonella typhimurium, Escherichia coli), two gram-positive bacteria (Bacillus cereus, Staphylococcus aureus), and one yeast like fungi (Candida albicans). The antimicrobial activity was analyzed using the well diffusion method, where zones of inhibition were used as indicators of antimicrobial activity.
Results and conclusion The venom exhibited notable antimicrobial activity against all tested pathogens. Gram-positive bacterial strains were found to be more sensitive than both gram-negative bacterial strains and fungal strain. The highest inhibition zones were determined to be 24.3±1.9, 29.3±1.5, 17.3±1.8, 14.0±1.7, and 15.7±1.5 mm for S. aureus, B. cereus, S. typhimurium, E. coli, and C. albicans, respectively. The corresponding minimum inhibitory concentration values were determined to be 0.32, 0.16, 0.625, 1.25, and 0.625 mg/ml, respectively. These results offer insights into the antimicrobial potency of wasp venom and provide a basis for further pharmacological research.

Background and objectives Methomyl (MET) [S-methyl N-(methylcarbamoyloxy) thioacetimidate; C5H10N2O2S] is one of the most important carbamate (oximes) insecticides that is extensively used around the world. Carbamate compounds are known to cause an alteration in biochemical parameters and affect the oxidative status of the body through producing free radicals. Many antioxidants have been used to ameliorate the toxic effect of pesticides, but the search for such compounds will always be an urgent need to achieve the optimum degree of amelioration. For this purpose, the present study was designed to evaluate the ameliorating effect of green tea extract (GTE) (Camellia sinensis), sage extract (SE) (Salvia officinalis) and their mixture (GTE+SE) against MET-induced toxicity in male rats.
Materials and methods A total of 60 rats (Rattus norvegicus) were divided into 12 groups: one negative control group (water); three positive control groups (GTE, SE, and GTE+SE) as the sole drinking source throughout the experimental duration (28 days); two groups administered MET orally at a dose equivalent to the acceptable daily intake and 10× acceptable daily intake; two groups were specified for GTE with MET two doses; two groups for SE with MET two doses; and two groups for GTE+SE with MET two doses. At the end of the experiment, blood samples were collected for measuring biochemical parameters for liver and kidney, as well as antioxidant enzymes.
Results and conclusion The insecticide caused high elevation in aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, urea, creatinine and malondialdehyde levels, and high decline in the levels of butyrylcholinesterase, superoxide dismutase, and total antioxidant capacity. Alterations in these biochemical markers occurred in a dose-dependent manner and were referred to the oxidative stress induced by MET. Co-administration of GTE or SE in conjunction with MET brought most of the tested biochemical parameters to their normal levels, but the mixture (GTE+SE) resulted in superior ameliorating effects as compared with each of the individual extracts. The study introduced novel findings regarding to the protective effect of GTE, SE, and their mixture against MET-induced toxicity in rats.